DK2588086T3 - PHARMACEUTICAL COMPOSITIONS CONTAINING 4-AMINO-5-FLUORO-3- [6- (4-METHYLPIPERAZIN-1-YL) -1H-BENZIMIDAZOL-2-YL] -1H-QUINOLIN-2-ON-LACTATE MONOHYDRATE - Google Patents
PHARMACEUTICAL COMPOSITIONS CONTAINING 4-AMINO-5-FLUORO-3- [6- (4-METHYLPIPERAZIN-1-YL) -1H-BENZIMIDAZOL-2-YL] -1H-QUINOLIN-2-ON-LACTATE MONOHYDRATE Download PDFInfo
- Publication number
- DK2588086T3 DK2588086T3 DK11734043.0T DK11734043T DK2588086T3 DK 2588086 T3 DK2588086 T3 DK 2588086T3 DK 11734043 T DK11734043 T DK 11734043T DK 2588086 T3 DK2588086 T3 DK 2588086T3
- Authority
- DK
- Denmark
- Prior art keywords
- weight
- amount
- mixture
- benzimidazol
- methylpiperazin
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 title claims description 20
- QDPVYZNVVQQULH-UHFFFAOYSA-N 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one 2-hydroxypropanoic acid hydrate Chemical compound O.CC(O)C(O)=O.C1CN(C)CCN1C1=CC=C(N=C(N2)C=3C(NC4=CC=CC(F)=C4C=3N)=O)C2=C1 QDPVYZNVVQQULH-UHFFFAOYSA-N 0.000 title claims description 16
- 239000000203 mixture Substances 0.000 claims description 115
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 60
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 46
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 46
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 44
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 37
- 229960000913 crospovidone Drugs 0.000 claims description 37
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 37
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 37
- 235000019359 magnesium stearate Nutrition 0.000 claims description 30
- 238000009472 formulation Methods 0.000 claims description 28
- 239000000945 filler Substances 0.000 claims description 27
- 239000002775 capsule Substances 0.000 claims description 25
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 25
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 25
- 238000000034 method Methods 0.000 claims description 23
- 239000000314 lubricant Substances 0.000 claims description 17
- 239000000377 silicon dioxide Substances 0.000 claims description 16
- PIQCTGMSNWUMAF-UHFFFAOYSA-N chembl522892 Chemical compound C1CN(C)CCN1C1=CC=C(NC(=N2)C=3C(NC4=CC=CC(F)=C4C=3N)=O)C2=C1 PIQCTGMSNWUMAF-UHFFFAOYSA-N 0.000 claims description 13
- 239000007884 disintegrant Substances 0.000 claims description 13
- 239000008187 granular material Substances 0.000 claims description 12
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 10
- 229930195725 Mannitol Natural products 0.000 claims description 9
- 238000007906 compression Methods 0.000 claims description 9
- 230000006835 compression Effects 0.000 claims description 9
- 238000007908 dry granulation Methods 0.000 claims description 9
- 239000000594 mannitol Substances 0.000 claims description 9
- 235000010355 mannitol Nutrition 0.000 claims description 9
- 238000004519 manufacturing process Methods 0.000 claims description 8
- 238000012545 processing Methods 0.000 claims description 6
- 238000002156 mixing Methods 0.000 claims description 5
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- 238000007873 sieving Methods 0.000 claims description 3
- 230000015572 biosynthetic process Effects 0.000 claims description 2
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 claims description 2
- 239000002360 explosive Substances 0.000 claims 2
- 238000005461 lubrication Methods 0.000 claims 2
- 239000003826 tablet Substances 0.000 description 31
- -1 clays Polymers 0.000 description 24
- 150000001875 compounds Chemical class 0.000 description 20
- 238000004090 dissolution Methods 0.000 description 16
- 229910002012 Aerosil® Inorganic materials 0.000 description 10
- 239000004480 active ingredient Substances 0.000 description 10
- 239000000546 pharmaceutical excipient Substances 0.000 description 10
- 238000009490 roller compaction Methods 0.000 description 10
- 235000012239 silicon dioxide Nutrition 0.000 description 10
- 239000007963 capsule composition Substances 0.000 description 9
- 238000012360 testing method Methods 0.000 description 9
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 7
- 229920001531 copovidone Polymers 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 5
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 5
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 5
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 5
- 238000000634 powder X-ray diffraction Methods 0.000 description 5
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- 229920002785 Croscarmellose sodium Polymers 0.000 description 4
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- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 3
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 3
- 239000008186 active pharmaceutical agent Substances 0.000 description 3
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- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical class CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- BSYNFGPFPYSTTM-UHFFFAOYSA-N 2-hydroxypropanoic acid;hydrate Chemical compound O.CC(O)C(O)=O BSYNFGPFPYSTTM-UHFFFAOYSA-N 0.000 description 2
- ZRHDKBOBHHFLBW-UHFFFAOYSA-N 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one 2-hydroxypropanoic acid Chemical compound CC(O)C(O)=O.C1CN(C)CCN1C1=CC=C(NC(=N2)C=3C(NC4=CC=CC(F)=C4C=3N)=O)C2=C1 ZRHDKBOBHHFLBW-UHFFFAOYSA-N 0.000 description 2
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- BAPJBEWLBFYGME-UHFFFAOYSA-N Methyl acrylate Chemical compound COC(=O)C=C BAPJBEWLBFYGME-UHFFFAOYSA-N 0.000 description 2
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- 239000008351 acetate buffer Substances 0.000 description 2
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- 229940105329 carboxymethylcellulose Drugs 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000007922 dissolution test Methods 0.000 description 2
- 238000005538 encapsulation Methods 0.000 description 2
- 150000004676 glycans Chemical class 0.000 description 2
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 2
- 229960001855 mannitol Drugs 0.000 description 2
- 229940124531 pharmaceutical excipient Drugs 0.000 description 2
- 229920001282 polysaccharide Polymers 0.000 description 2
- 239000005017 polysaccharide Substances 0.000 description 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
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- 239000000126 substance Substances 0.000 description 2
- 239000007916 tablet composition Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- LPBRRMTWKXOQDO-UHFFFAOYSA-N 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one 2-hydroxypropanoic acid hydrate Chemical compound O.C(C(O)C)(=O)O.C(C(O)C)(=O)O.NC1=C(C(NC2=CC=CC(=C12)F)=O)C1=NC2=C(N1)C=C(C=C2)N2CCN(CC2)C LPBRRMTWKXOQDO-UHFFFAOYSA-N 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 229920000623 Cellulose acetate phthalate Polymers 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- 229920003134 Eudragit® polymer Polymers 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 229920002907 Guar gum Polymers 0.000 description 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 229920002845 Poly(methacrylic acid) Polymers 0.000 description 1
- 229920002319 Poly(methyl acrylate) Polymers 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 229920003081 Povidone K 30 Polymers 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
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- 235000002017 Zea mays subsp mays Nutrition 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- CEGOLXSVJUTHNZ-UHFFFAOYSA-K aluminium tristearate Chemical compound [Al+3].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CEGOLXSVJUTHNZ-UHFFFAOYSA-K 0.000 description 1
- 229940063655 aluminum stearate Drugs 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 description 1
- 239000008116 calcium stearate Substances 0.000 description 1
- 235000013539 calcium stearate Nutrition 0.000 description 1
- 229920002301 cellulose acetate Polymers 0.000 description 1
- 229940081734 cellulose acetate phthalate Drugs 0.000 description 1
- 239000008119 colloidal silica Substances 0.000 description 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 238000005056 compaction Methods 0.000 description 1
- 235000005822 corn Nutrition 0.000 description 1
- 229920006037 cross link polymer Polymers 0.000 description 1
- 239000001767 crosslinked sodium carboxy methyl cellulose Substances 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- FSBVERYRVPGNGG-UHFFFAOYSA-N dimagnesium dioxido-bis[[oxido(oxo)silyl]oxy]silane hydrate Chemical compound O.[Mg+2].[Mg+2].[O-][Si](=O)O[Si]([O-])([O-])O[Si]([O-])=O FSBVERYRVPGNGG-UHFFFAOYSA-N 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 239000013583 drug formulation Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 239000007941 film coated tablet Substances 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000000665 guar gum Substances 0.000 description 1
- 235000010417 guar gum Nutrition 0.000 description 1
- 229960002154 guar gum Drugs 0.000 description 1
- 230000036571 hydration Effects 0.000 description 1
- 238000006703 hydration reaction Methods 0.000 description 1
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 150000003893 lactate salts Chemical class 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 239000000395 magnesium oxide Substances 0.000 description 1
- CPLXHLVBOLITMK-UHFFFAOYSA-N magnesium oxide Inorganic materials [Mg]=O CPLXHLVBOLITMK-UHFFFAOYSA-N 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 229940099273 magnesium trisilicate Drugs 0.000 description 1
- 229910000386 magnesium trisilicate Inorganic materials 0.000 description 1
- 235000019793 magnesium trisilicate Nutrition 0.000 description 1
- AXZKOIWUVFPNLO-UHFFFAOYSA-N magnesium;oxygen(2-) Chemical compound [O-2].[Mg+2] AXZKOIWUVFPNLO-UHFFFAOYSA-N 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229920003124 powdered cellulose Polymers 0.000 description 1
- 235000019814 powdered cellulose Nutrition 0.000 description 1
- 238000012776 robust process Methods 0.000 description 1
- 239000008279 sol Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- OIWCYIUQAVBPGV-DAQGAKHBSA-N {1-O-hexadecanoyl-2-O-[(Z)-octadec-9-enoyl]-sn-glycero-3-phospho}serine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(=O)OC[C@H](N)C(O)=O)OC(=O)CCCCCCC\C=C/CCCCCCCC OIWCYIUQAVBPGV-DAQGAKHBSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10168028 | 2010-06-30 | ||
| PCT/EP2011/060949 WO2012001074A2 (en) | 2010-06-30 | 2011-06-29 | Pharmaceutical compositions comprising 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one lactate monohydrate. |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| DK2588086T3 true DK2588086T3 (en) | 2019-01-07 |
Family
ID=42751565
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DK11734043.0T DK2588086T3 (en) | 2010-06-30 | 2011-06-29 | PHARMACEUTICAL COMPOSITIONS CONTAINING 4-AMINO-5-FLUORO-3- [6- (4-METHYLPIPERAZIN-1-YL) -1H-BENZIMIDAZOL-2-YL] -1H-QUINOLIN-2-ON-LACTATE MONOHYDRATE |
Country Status (37)
| Country | Link |
|---|---|
| US (1) | US9545402B2 (es) |
| EP (2) | EP2588086B1 (es) |
| JP (1) | JP6043281B2 (es) |
| KR (2) | KR20130091319A (es) |
| CN (2) | CN106943355B (es) |
| AR (1) | AR081776A1 (es) |
| AU (1) | AU2011273519B2 (es) |
| BR (1) | BR112012033479A8 (es) |
| CA (1) | CA2801826C (es) |
| CL (1) | CL2012003729A1 (es) |
| CO (1) | CO6650354A2 (es) |
| CR (1) | CR20120623A (es) |
| CU (1) | CU20120177A7 (es) |
| DK (1) | DK2588086T3 (es) |
| DO (1) | DOP2012000324A (es) |
| EA (1) | EA026244B1 (es) |
| EC (1) | ECSP13012411A (es) |
| ES (1) | ES2701161T3 (es) |
| GE (1) | GEP20146049B (es) |
| GT (1) | GT201200348A (es) |
| HU (1) | HUE042355T2 (es) |
| IL (1) | IL223799A (es) |
| MA (1) | MA34387B1 (es) |
| MX (1) | MX345404B (es) |
| MY (2) | MY163369A (es) |
| NI (1) | NI201200189A (es) |
| NZ (1) | NZ604055A (es) |
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Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2013063003A1 (en) | 2011-10-28 | 2013-05-02 | Novartis Ag | Method of treating gastrointestinal stromal tumors |
| EP2809312A1 (en) | 2012-01-31 | 2014-12-10 | Novartis AG | Combination of a rtk inhibitor with an anti - estrogen and use thereof for the treatment of cancer |
| IN2014DN10801A (es) | 2012-07-11 | 2015-09-04 | Novartis Ag | |
| US9395468B2 (en) | 2012-08-27 | 2016-07-19 | Ocular Dynamics, Llc | Contact lens with a hydrophilic layer |
| WO2014058785A1 (en) | 2012-10-10 | 2014-04-17 | Novartis Ag | Combination therapy |
| US9492535B2 (en) | 2013-03-14 | 2016-11-15 | Aimmune Therapeutics, Inc. | Peanut formulations and uses thereof |
| DK3482771T3 (da) * | 2013-03-14 | 2023-03-20 | Nestle Sa | Fremstilling af jordnøddeformuleringer til oral desensibilisering |
| EP3988992A1 (en) | 2013-11-15 | 2022-04-27 | Tangible Science, Inc. | Contact lens with a hydrophilic layer |
| WO2015187736A1 (en) * | 2014-06-02 | 2015-12-10 | Allergen Research Corporation | Placebo formulations and uses thereof |
| AU2015360637B2 (en) | 2014-12-09 | 2019-08-22 | Tangible Science, Inc. | Medical device coating with a biocompatible layer |
| TWI790189B (zh) | 2015-01-02 | 2023-01-21 | 美商梅拉洛伊卡公司 | 細菌組成物 |
| AU2016268477B2 (en) * | 2015-05-22 | 2018-12-20 | Novartis Ag | Pharmaceutical compositions |
| US11369676B2 (en) | 2017-11-02 | 2022-06-28 | Société des Produits Nestlé S.A. | Methods of oral immunotherapy |
| CA3137295A1 (en) | 2019-05-10 | 2020-11-19 | Aimmune Therapeutics, Inc. | Methods for improving the quality of life of a patient with a peanut allergy |
| US10835531B1 (en) | 2019-06-18 | 2020-11-17 | Oncology Venture ApS | Methods for predicting drug responsiveness in cancer patients |
| US20230302139A1 (en) * | 2020-07-31 | 2023-09-28 | University Of Florida Research Foundation, Incorporated | Targeted rna degradation allows precision repurposing of protein-targeted small molecule medicines to rna |
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| US5009897A (en) * | 1988-06-24 | 1991-04-23 | Abbott Laboratories | Pharmaceutical granules and tablets made therefrom |
| EP1650203B1 (en) | 2000-09-11 | 2008-02-20 | Novartis Vaccines and Diagnostics, Inc. | Process of preparation of benzimidazol-2-yl quinolinone derivatives |
| AU2003288899B2 (en) | 2002-08-23 | 2009-09-03 | Novartis Vaccines And Diagnostics, Inc. | Benzimidazole quinolinones and uses thereof |
| US20060172006A1 (en) * | 2003-10-10 | 2006-08-03 | Vincent Lenaerts | Sustained-release tramadol formulations with 24-hour clinical efficacy |
| GB0504203D0 (en) * | 2005-03-01 | 2005-04-06 | Novartis Ag | Organic compounds |
| WO2006127926A2 (en) * | 2005-05-23 | 2006-11-30 | Novartis Ag | Crystalline and other forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one lactic acid salts |
| CA2615063A1 (en) * | 2005-07-22 | 2007-02-01 | Myriad Genetics, Inc. | High drug load formulations and dosage forms |
| CN101316593B (zh) * | 2005-11-29 | 2012-05-02 | 诺瓦提斯公司 | 喹啉酮类的制剂 |
| MY148529A (en) | 2005-11-29 | 2013-04-30 | Novartis Ag | Formulations of quinolinones |
| RU2009136669A (ru) | 2007-03-09 | 2011-04-20 | Новартис АГ (CH) | Лечение меланомы |
| KR20150105494A (ko) | 2007-11-08 | 2015-09-16 | 암비트 바이오사이언시즈 코포레이션 | 증식성 질환을 치료하기 위하여 ｎ－（5－ｔｅｒｔ－부틸－아이소제이졸－3－일）－ｎ′－｛4－［7－（2－몰포린－4－일－에톡시）이미다조［2,1－ｂ］［1,3］벤조티아졸－2－일］페닐｝우레아를 투여하는 방법 |
| PE20091628A1 (es) | 2008-03-19 | 2009-11-19 | Novartis Ag | Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona |
| EP2108365A1 (en) * | 2008-04-09 | 2009-10-14 | LEK Pharmaceuticals d.d. | Single dosage pharmaceutical formulation comprising eprosartan mesylate |
| NZ602807A (en) | 2010-04-16 | 2014-02-28 | Novartis Ag | 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one and an mtor inhibitor |
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